{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,14]],"date-time":"2026-09-14T11:04:05Z","timestamp":1789383845254,"version":"build-2803163510"},"reference-count":47,"publisher":"Elsevier BV","issue":"8","license":[{"start":{"date-parts":[[2026,8,1]],"date-time":"2026-08-01T00:00:00Z","timestamp":1785542400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2026,8,1]],"date-time":"2026-08-01T00:00:00Z","timestamp":1785542400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2027,8,31]],"date-time":"2027-08-31T00:00:00Z","timestamp":1819670400000},"content-version":"am","delay-in-days":395,"URL":"http:\/\/www.elsevier.com\/open-access\/userlicense\/1.0\/"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000057","name":"National Institute of General Medical Sciences","doi-asserted-by":"publisher","award":["T32-GM145445"],"award-info":[{"award-number":["T32-GM145445"]}],"id":[{"id":"10.13039\/100000057","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["molpharm.aspetjournals.org","elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["Molecular Pharmacology"],"published-print":{"date-parts":[[2026,8]]},"DOI":"10.1016\/j.molpha.2026.100146","type":"journal-article","created":{"date-parts":[[2026,7,24]],"date-time":"2026-07-24T23:35:15Z","timestamp":1784936115000},"page":"100146","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":0,"title":["Panoramic characterization of proposed ligands for GPR3: oleoylethanolamide as a pharmacological chaperone"],"prefix":"10.1016","volume":"108","author":[{"ORCID":"https:\/\/orcid.org\/0000-0001-9924-3253","authenticated-orcid":false,"given":"Ian T.","family":"Pyne","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-5872-6344","authenticated-orcid":false,"given":"Alex J.","family":"Roy","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0001-8474-1492","authenticated-orcid":false,"given":"Sophia","family":"Boraschi","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0001-3745-0166","authenticated-orcid":false,"given":"Sanjit S.","family":"Hajgude","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8318-8728","authenticated-orcid":false,"given":"Randy A.","family":"Hall","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib1","doi-asserted-by":"crossref","first-page":"300","DOI":"10.1038\/s41401-018-0031-9","article-title":"GPR3, GPR6, and GPR12 as novel molecular targets: their biological functions and interaction with cannabidiol","volume":"40","author":"Laun","year":"2019","journal-title":"Acta Pharmacol Sin"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib2","doi-asserted-by":"crossref","first-page":"837","DOI":"10.1042\/bj3090837","article-title":"Molecular cloning of an orphan G-protein-coupled receptor that constitutively activates adenylate cyclase","volume":"309","author":"Eggerickx","year":"1995","journal-title":"Biochem J"},{"issue":"9","key":"10.1016\/j.molpha.2026.100146_bib3","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0138463","article-title":"Constitutive activity among orphan class-A G protein coupled receptors","volume":"10","author":"Martin","year":"2015","journal-title":"PLoS One"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib4","doi-asserted-by":"crossref","first-page":"74","DOI":"10.1080\/03602532.2018.1428616","article-title":"Towards a better understanding of the cannabinoid-related orphan receptors GPR3, GPR6, and GPR12","volume":"50","author":"Morales","year":"2018","journal-title":"Drug Metab Rev"},{"issue":"40","key":"10.1016\/j.molpha.2026.100146_bib5","doi-asserted-by":"crossref","DOI":"10.1073\/pnas.2204828119","article-title":"G protein\u2013biased GPR3 signaling ameliorates amyloid pathology in a preclinical Alzheimer's disease mouse model","volume":"119","author":"Huang","year":"2022","journal-title":"Proc Natl Acad Sci U S A"},{"issue":"309","key":"10.1016\/j.molpha.2026.100146_bib6","doi-asserted-by":"crossref","DOI":"10.1126\/scitranslmed.aab3492","article-title":"Loss of GPR3 reduces the amyloid plaque burden and improves memory in Alzheimer's disease mouse models","volume":"7","author":"Huang","year":"2015","journal-title":"Sci Transl Med"},{"issue":"9","key":"10.1016\/j.molpha.2026.100146_bib7","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0074680","article-title":"Gpr3 stimulates A\u03b2 production via interactions with APP and \u03b2-arrestin2","volume":"8","author":"Nelson","year":"2013","journal-title":"PLoS One"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib8","doi-asserted-by":"crossref","first-page":"43","DOI":"10.1038\/nm.3023","article-title":"\u03b2-arrestin 2 regulates A\u03b2 generation and \u03b3-secretase activity in Alzheimers disease","volume":"19","author":"Thathiah","year":"2013","journal-title":"Nat Med"},{"issue":"5916","key":"10.1016\/j.molpha.2026.100146_bib9","doi-asserted-by":"crossref","first-page":"946","DOI":"10.1126\/science.1160649","article-title":"The orphan G protein\u2013coupled receptor 3 modulates amyloid-beta peptide generation in neurons","volume":"323","author":"Thathiah","year":"2009","journal-title":"Science"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib10","doi-asserted-by":"crossref","DOI":"10.1038\/s41598-018-29475-7","article-title":"Allosteric sodium binding cavity in GPR3: a novel player in modulation of A\u03b2 production","volume":"8","author":"Capaldi","year":"2018","journal-title":"Sci Rep"},{"issue":"2","key":"10.1016\/j.molpha.2026.100146_bib11","doi-asserted-by":"crossref","first-page":"255","DOI":"10.1083\/jcb.200506194","article-title":"Regulation of meiotic prophase arrest in mouse oocytes by GPR3, a constitutive activator of the Gs G protein","volume":"171","author":"Freudzon","year":"2005","journal-title":"J Cell Biol"},{"issue":"2","key":"10.1016\/j.molpha.2026.100146_bib12","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1016\/j.ydbio.2005.08.019","article-title":"The G-protein-coupled receptors GPR3 and GPR12 are involved in cAMP signaling and maintenance of meiotic arrest in rodent oocytes","volume":"287","author":"Hinckley","year":"2005","journal-title":"Dev Biol"},{"issue":"5703","key":"10.1016\/j.molpha.2026.100146_bib13","doi-asserted-by":"crossref","first-page":"1947","DOI":"10.1126\/science.1103974","article-title":"The Gs-linked receptor GPR3 maintains meiotic arrest in mammalian oocytes","volume":"306","author":"Mehlmann","year":"2004","journal-title":"Science"},{"key":"10.1016\/j.molpha.2026.100146_bib14","doi-asserted-by":"crossref","DOI":"10.1038\/srep14953","article-title":"Mice lacking GPR3 receptors display late-onset obese phenotype due to impaired thermogenic function in brown adipose tissue","volume":"5","author":"Godlewski","year":"2015","journal-title":"Sci Rep"},{"issue":"13","key":"10.1016\/j.molpha.2026.100146_bib15","doi-asserted-by":"crossref","first-page":"3502","DOI":"10.1016\/j.cell.2021.04.037","article-title":"Lipolysis drives expression of the constitutively active receptor GPR3 to induce adipose thermogenesis","volume":"184","author":"Sveidahl Johansen","year":"2021","journal-title":"Cell"},{"key":"10.1016\/j.molpha.2026.100146_bib16","article-title":"Cold exposure induces the constitutively active thermogenic receptor, GPR3, via ERR\u03b1 and ERR\u03b3","volume":"103","author":"Sveidahl Johansen","year":"2025","journal-title":"Mol Metab"},{"issue":"9","key":"10.1016\/j.molpha.2026.100146_bib17","doi-asserted-by":"crossref","DOI":"10.1016\/j.jbc.2025.110571","article-title":"Constitutively active orphan G protein-coupled receptors through the lenses of cryo-electron microscopy","volume":"301","author":"Argerich","year":"2025","journal-title":"J Biol Chem"},{"issue":"11","key":"10.1016\/j.molpha.2026.100146_bib18","doi-asserted-by":"crossref","first-page":"941","DOI":"10.1016\/S0898-6568(02)00041-4","article-title":"Sphingosine 1-phosphate is a ligand of the human gpr3, gpr6 and gpr12 family of constitutively active G protein-coupled receptors","volume":"14","author":"Uhlenbrock","year":"2002","journal-title":"Cell Signal"},{"key":"10.1016\/j.molpha.2026.100146_bib19","doi-asserted-by":"crossref","DOI":"10.1016\/j.bmcl.2023.129427","article-title":"The development of diphenyleneiodonium analogs as GPR3 agonists","volume":"94","author":"Gay","year":"2023","journal-title":"Bioorg Med Chem Lett"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib20","doi-asserted-by":"crossref","first-page":"437","DOI":"10.1124\/jpet.114.213082","article-title":"Identification of a novel small-molecule agonist for human G protein\u2013coupled receptor 3","volume":"349","author":"Ye","year":"2014","journal-title":"J Pharmacol Exp Ther"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib21","doi-asserted-by":"crossref","first-page":"262","DOI":"10.1038\/s41422-023-00919-8","article-title":"Structural and functional characterization of the endogenous agonist for orphan receptor GPR3","volume":"34","author":"Chen","year":"2024","journal-title":"Cell Res"},{"issue":"5","key":"10.1016\/j.molpha.2026.100146_bib22","doi-asserted-by":"crossref","first-page":"625","DOI":"10.1021\/acs.biochem.3c00647","article-title":"Lipid-dependent activation of the orphan G protein-coupled receptor, GPR3","volume":"63","author":"Russell","year":"2024","journal-title":"Biochemistry"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib23","doi-asserted-by":"crossref","first-page":"232","DOI":"10.1038\/s41422-024-00932-5","article-title":"Identification of oleic acid as an endogenous ligand of GPR3","volume":"34","author":"Xiong","year":"2024","journal-title":"Cell Res"},{"issue":"4","key":"10.1016\/j.molpha.2026.100146_bib24","doi-asserted-by":"crossref","DOI":"10.1016\/j.celrep.2025.115478","article-title":"Structural basis of oligomerization-modulated activation and autoinhibition of orphan receptor GPR3","volume":"44","author":"Chang","year":"2025","journal-title":"Cell Rep"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib25","doi-asserted-by":"crossref","first-page":"7988","DOI":"10.1038\/s41467-025-63422-1","article-title":"Mechanism and function of GPR3 regulated by a negative allosteric modulator","volume":"16","author":"Chen","year":"2025","journal-title":"Nat Commun"},{"key":"10.1016\/j.molpha.2026.100146_bib26","article-title":"Allosteric modulation of dimeric GPR3 by ligands in the dimerization interface","author":"Qiu","year":"2025","journal-title":"Preprint"},{"issue":"21","key":"10.1016\/j.molpha.2026.100146_bib27","doi-asserted-by":"crossref","first-page":"15025","DOI":"10.1021\/acs.jmedchem.3c01707","article-title":"Development of fluorescent AF64394 analogues enables real-time binding studies for the orphan class A GPCR GPR3","volume":"66","author":"Bresinsky","year":"2023","journal-title":"J Med Chem"},{"issue":"22","key":"10.1016\/j.molpha.2026.100146_bib28","doi-asserted-by":"crossref","first-page":"5195","DOI":"10.1016\/j.bmcl.2014.09.077","article-title":"The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function","volume":"24","author":"Jensen","year":"2014","journal-title":"Bioorg Med Chem Lett"},{"issue":"20","key":"10.1016\/j.molpha.2026.100146_bib29","doi-asserted-by":"crossref","first-page":"10181","DOI":"10.1080\/07391102.2021.1940282","article-title":"Structural basis for the binding of a selective inverse agonist AF64394 with the human G-protein coupled receptor 3 (GPR3)","volume":"40","author":"Bharathi","year":"2022","journal-title":"J Biomol Struct Dyn"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib30","doi-asserted-by":"crossref","first-page":"17","DOI":"10.1016\/j.bbrc.2017.05.165","article-title":"GPR3 and GPR6, novel molecular targets for cannabidiol","volume":"490","author":"Laun","year":"2017","journal-title":"Biochem Biophys Res Commun"},{"key":"10.1016\/j.molpha.2026.100146_bib31","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1016\/j.ymeth.2021.10.009","article-title":"Luciferase-based GloSensor\u2122 cAMP assay: temperature optimization and application to cell-based kinetic studies","volume":"203","author":"Wang","year":"2022","journal-title":"Methods"},{"key":"10.1016\/j.molpha.2026.100146_bib32","series-title":"Methods in Cell Biology","first-page":"131","article-title":"Measuring surface expression and endocytosis of GPCRs using whole-cell ELISA","author":"Pandey","year":"2019"},{"issue":"45","key":"10.1016\/j.molpha.2026.100146_bib33","doi-asserted-by":"crossref","first-page":"32248","DOI":"10.1074\/jbc.274.45.32248","article-title":"Association of \u03b2-arrestin with G protein-coupled receptors during clathrin-mediated endocytosis dictates the profile of receptor resensitization","volume":"274","author":"Oakley","year":"1999","journal-title":"J Biol Chem"},{"issue":"1","key":"10.1016\/j.molpha.2026.100146_bib34","doi-asserted-by":"crossref","first-page":"1","DOI":"10.1016\/S0031-6997(24)01478-9","article-title":"Evolving concepts in G protein-coupled receptor endocytosis: the role in receptor desensitization and signaling","volume":"53","author":"Ferguson","year":"2001","journal-title":"Pharmacol Rev"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib35","doi-asserted-by":"crossref","first-page":"167","DOI":"10.1016\/j.cmet.2006.02.004","article-title":"Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule hypophagic agents","volume":"3","author":"Overton","year":"2006","journal-title":"Cell Metab"},{"issue":"5","key":"10.1016\/j.molpha.2026.100146_bib36","doi-asserted-by":"crossref","first-page":"1058","DOI":"10.2337\/db08-1237","article-title":"GPR119 is essential for oleoylethanolamide-induced glucagon-like peptide-1 secretion from the intestinal enteroendocrine L-cell","volume":"58","author":"Lauffer","year":"2009","journal-title":"Diabetes"},{"issue":"6655","key":"10.1016\/j.molpha.2026.100146_bib37","doi-asserted-by":"crossref","first-page":"88","DOI":"10.1038\/36362","article-title":"Switching of the coupling of the \u03b22-adrenergic receptor to different G proteins by protein kinase A","volume":"390","author":"Daaka","year":"1997","journal-title":"Nature"},{"issue":"2","key":"10.1016\/j.molpha.2026.100146_bib38","doi-asserted-by":"crossref","first-page":"1261","DOI":"10.1074\/jbc.M506576200","article-title":"\u03b2-arrestin-dependent, G protein-independent ERK1\/2 activation by the \u03b22 adrenergic receptor","volume":"281","author":"Shenoy","year":"2006","journal-title":"J Biol Chem"},{"issue":"11","key":"10.1016\/j.molpha.2026.100146_bib39","doi-asserted-by":"crossref","first-page":"2881","DOI":"10.1096\/fasebj.4.11.2165947","article-title":"Turning off the signal: desensitization of \u03b2-adrenergic receptor function","volume":"4","author":"Hausdorff","year":"1990","journal-title":"FASEB J"},{"issue":"2","key":"10.1016\/j.molpha.2026.100146_bib40","doi-asserted-by":"crossref","first-page":"563","DOI":"10.1124\/jpet.106.105221","article-title":"Pharmacological characterization of hydrolysis-resistant analogs of oleoylethanolamide with potent anorexiant properties","volume":"318","author":"Astarita","year":"2006","journal-title":"J Pharmacol Exp Ther"},{"issue":"6599","key":"10.1016\/j.molpha.2026.100146_bib41","doi-asserted-by":"crossref","first-page":"447","DOI":"10.1038\/383447a0","article-title":"\u03b2-Arrestin acts as a clathrin adaptor in endocytosis of the \u03b22-adrenergic receptor","volume":"383","author":"Goodman","year":"1996","journal-title":"Nature"},{"issue":"5","key":"10.1016\/j.molpha.2026.100146_bib42","doi-asserted-by":"crossref","first-page":"222","DOI":"10.1016\/j.tem.2004.05.003","article-title":"Pharmacological chaperones: potential treatment for conformational diseases","volume":"15","author":"Bernier","year":"2004","journal-title":"Trends Endocrinol Metab"},{"issue":"2","key":"10.1016\/j.molpha.2026.100146_bib43","doi-asserted-by":"crossref","first-page":"697","DOI":"10.1152\/physrev.00029.2016","article-title":"Pharmacoperones as novel therapeutics for diverse protein conformational diseases","volume":"98","author":"Tao","year":"2018","journal-title":"Physiol Rev"},{"issue":"31","key":"10.1016\/j.molpha.2026.100146_bib44","doi-asserted-by":"crossref","first-page":"21995","DOI":"10.1016\/S0021-9258(18)41623-7","article-title":"Enhancement of membrane insertion and function in a type IIIb membrane protein following introduction of a cleavable signal peptide","volume":"267","author":"Guan","year":"1992","journal-title":"J Biol Chem"},{"issue":"9","key":"10.1016\/j.molpha.2026.100146_bib45","doi-asserted-by":"crossref","first-page":"541","DOI":"10.1016\/j.tibtech.2009.06.005","article-title":"Enhancement of the surface expression of G protein-coupled receptors","volume":"27","author":"Dunham","year":"2009","journal-title":"Trends Biotechnol"},{"issue":"3","key":"10.1016\/j.molpha.2026.100146_bib46","doi-asserted-by":"crossref","first-page":"307","DOI":"10.1016\/j.jphs.2022.01.005","article-title":"Potential role of inducible GPR3 expression under stimulated T cell conditions","volume":"148","author":"Shiraki","year":"2022","journal-title":"J Pharmacol Sci"},{"issue":"5","key":"10.1016\/j.molpha.2026.100146_bib47","doi-asserted-by":"crossref","first-page":"1216","DOI":"10.1016\/j.cell.2014.03.058","article-title":"Npas4 regulates excitatory-inhibitory balance within neural circuits through cell-type-specific gene programs","volume":"157","author":"Spiegel","year":"2014","journal-title":"Cell"}],"container-title":["Molecular Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0026895X26000465?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0026895X26000465?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2026,9,14]],"date-time":"2026-09-14T10:10:39Z","timestamp":1789380639000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0026895X26000465"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,8]]},"references-count":47,"journal-issue":{"issue":"8","published-print":{"date-parts":[[2026,8]]}},"alternative-id":["S0026895X26000465"],"URL":"https:\/\/doi.org\/10.1016\/j.molpha.2026.100146","relation":{},"ISSN":["0026-895X"],"issn-type":[{"value":"0026-895X","type":"print"}],"subject":[],"published":{"date-parts":[[2026,8]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Panoramic characterization of proposed ligands for GPR3: oleoylethanolamide as a pharmacological chaperone","name":"articletitle","label":"Article Title"},{"value":"Molecular Pharmacology","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.molpha.2026.100146","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2026 American Society for Pharmacology and Experimental Therapeutics. Published by Elsevier Inc. All rights are reserved, including those for text and data mining, AI training, and similar technologies.","name":"copyright","label":"Copyright"}],"article-number":"100146"}}